51486-03-4Relevant academic research and scientific papers
Synthesis and cytotoxic activity of chalcone analogues containing a thieno[2,3-d]pyrimidin-2-yl group as the A-ring or B-ring
Wang, Fu-Cheng,Peng, Bin,Cao, Sheng-Li,Li, Hong-Yun,Yuan, Xiao-Li,Zhang, Ting-Ting,Shi, Ruifeng,Li, Zhuqing,Liao, Ji,Wang, Hailong,Li, Jing,Xu, Xingzhi
, (2019/11/03)
Many natural or synthetic chalcones have potential anti-tumor activity. Here, we synthesized two series of chalcone analogues containing a thieno[2,3-d]pyrimidin-2-yl group and evaluated for their cytotoxic activity towards cultured human lung cancer A549 and colorectal HCT-116 cells. Among them, compound 8d was the most cytotoxic against HCT-116 cells, with an IC50 value of 2.65 μM. Analyses of the phenotypic changes induced by this compound found a dose-dependent accumulation of HCT-116 cells in sub-G1 phase, indicating that compound 8d might induce apoptosis. Furthermore, we found that 8d triggered mitochondrial membrane potential depolarization, promoted reactive oxygen species formation in HCT-116 cells, and increased the percentage of early and late apoptotic cells. Finally, immunoblotting indicated that 8d increased PARP-1 and caspases 3, 7 and 9 cleavage. These data suggest that compound 8d induces apoptosis via the mitochondrial death pathway.
Chalcone analogue containing thieno[2,3-d]pyrimidine-2-yl, preparation method and uses thereof
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Paragraph 0100; 0101; 0103, (2020/01/03)
The invention discloses a chalcone analogue containing thieno[2,3-d]pyrimidine-2-yl, wherein the chalcone analogue is represented by a general formula (I), and various substituents are defined in thespecification. The invention further discloses a preparation method of the compound. According to the present invention, the compound represented by the general formula (I) has inhibiting effects on the proliferation of human breast cancer cell lines (MFC-7 and MDA-MB-231), human cervical cancer cell lines (HeLa), human colon cancer cell lines (HCT-116 and HT-29) and human lung cancer cell lines (A549), has inhibiting effect on the proliferation of human hepatoma cell lines (HepG2), and can be used as an antitumor drug.
THIENOPYRIDINE AND THIENOPYRIMIDINE COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 99, (2012/03/26)
Provided herein are thienopyridine and thienopyrimidine compounds of formula (I) for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising
NOVEL THIENO-PYRIDINE AND THIENO-PYRIMIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2-RECEPTORS
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Page/Page column 57, (2010/10/20)
The present invention relates to novel compounds, in particular novel thieno-pyridine and thieno-pyrimidine derivatives according to Formula (I), wherein all radicals are defined in the application. The compounds according to the invention are positive al
NOVEL HERBICIDES, USAGE THEREOF, NOVEL THIENOPYRIMIDINE DERIVATIVES, INTERMEDIATES OF THE SAME, AND PROCESS FOR PRODUCTION THEREOF
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Page/Page column 51, (2010/02/12)
A herbicide comprising, as an active ingredient, a substituted thienopyrimidine derivative represented by the formula (I): wherein all symbols are defined in the description, a method of using the same, a novel compound useful as the herbicide and a process for producing the same, and an intermediate thereof.
PSYCHOTROPIC HETEROBICYCLOALKYLPIPERAZINE DERIVATIVES
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, (2008/06/13)
A series of psychotropic heterobicycloalkylpiperazine derivatives having the structure STR1 wherein V is a 3-or 4-membered unsaturated chain, containing all carbon atoms when 4-membered, or when a 3-membered chain, V contains an oxygen or sulfur atom as one of the members; R is H or C 1-4 alkyl; W is CH, N, CH 2, or a chemical bond; X is CH, N, SO 2, or CO, with the proviso that both W and X cannot simultaneously be N; and Z is a heteroaromatic ring system. These compounds are useful antipsychotic and/or anxiolytic agents.
